公开(公告)号：US4150139A

公开(公告)日：1979-04-17

申请号：US821623

申请日：1977-08-03

申请人： Yutaka Kuwada ,  Hiroyuki Tawada

发明人： Yutaka Kuwada ,  Hiroyuki Tawada

IPC分类号： C07D249/12 ,  C07D487/04 ,  A61K31/55

CPC分类号： C07D487/04 ,  C07D249/12

摘要： Novel triazolobenzazepine derivatives of the formula ##STR1## (wherein R.sup.1 and R.sup.2 are hydrogen or alkyl, X is ##STR2## wherein R.sup.3 and R.sup.4 are hydrogen, alkyl, aryl or aralkyl, and R.sup.5 is hydrogen or alkyl), Z is --SR.sup.6, --S(O).sub.n R.sup.6 or --OR.sup.7 (wherein R.sup.6 and R.sup.7 are alkyl or aralkyl, and n is 1 or 2), and Ring A is unsubstituted or substituted with at least one of halogen, lower alkyl, lower alkoxy and trifluoromethyl, and their physiologically acceptable salts have excellent pharmacological activities and are useful as medicines such as muscle-relaxants, analgesics and antiinflammatory drugs.

摘要翻译： 式（IMA）的新型三唑并苯并吖庚因衍生物（其中R 1和R 2是氢或烷基，X是其中R 3和R 4是氢，烷基，芳基或芳烷基，R 5是氢或烷基），Z是-SR 6， -S（O）n R 6或-OR 7（其中R 6和R 7为烷基或芳烷基，n为1或2），环A为未取代的或被至少一个卤素，低级烷基，低级烷氧基和三氟甲基取代，以及 其生理上可接受的盐具有优异的药理活性，并且可用作药物如肌肉松弛剂，止痛剂和抗炎药。

公开(公告)号：US4463172A

公开(公告)日：1984-07-31

申请号：US235998

申请日：1981-02-19

申请人： Satoshi Horii ,  Nariakira Mizokami ,  Yutaka Kuwada

发明人： Satoshi Horii ,  Nariakira Mizokami ,  Yutaka Kuwada

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  C07D501/04 ,  C07D501/14 ,  C07D501/16 ,  C07D501/18 ,  C07D501/36 ,  C07D501/60

CPC分类号： C07D501/04 ,  C07D501/14

摘要： Novel 2-methylcephalosporin derivatives and production thereof. These cephalosporin derivatives exhibit excellent antibacterial activities against gram-positive and gram-negative bacteria, thus being of value as a prophylactic or therapeutic agent for infections observed in man and animals.

摘要翻译： 新型2-甲基头孢菌素衍生物及其制备方法。 这些头孢菌素衍生物对革兰氏阳性菌和革兰氏阴性细菌表现出优异的抗菌活性，因此作为在人和动物中观察到的感染的预防或治疗剂是有价值的。

公开(公告)号：US4145418A

公开(公告)日：1979-03-20

申请号：US755428

申请日：1976-12-29

申请人： Yutaka Kuwada ,  Kanji Meguro

发明人： Yutaka Kuwada ,  Kanji Meguro

IPC分类号： C07D499/00 ,  C07D499/64 ,  C07D499/68 ,  C07D501/20 ,  C07D501/36 ,  A61K31/545

CPC分类号： C07D499/00

摘要： Thienopyridine derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each is hydrogen, an alkyl, an aryl, an aralkyl or a halogen; R.sup.1 and R.sup.2 may, taken together, represent an alkylene group; X is hydrogen or an alkyl; Y is oxygen or sulfur; Z is phenyl which may optionally be substituted; R.sup.3 is hydrogen or an alkoxy; and R is a group of the formula: ##STR2## or of the formula: ##STR3## (wherein R.sup.4 is hydrogen, an acyloxy or a nucleophilic compound residue) or a pharmaceutically acceptable salt thereof are found to have activity against a broad spectrum of gram-positive and gram-negative bacteria, particularly against bacteria of the genus Pseudomonas .

公开(公告)号：US4116956A

公开(公告)日：1978-09-26

申请号：US718194

申请日：1976-08-26

申请人： Kanji Meguro ,  Yutaka Kuwada

发明人： Kanji Meguro ,  Yutaka Kuwada

IPC分类号： C07D243/20

CPC分类号： C07D243/20 ,  Y10S514/906

摘要： Benzodiazepine derivatives of the general formula ##STR1## where R.sub.1 is hydrogen or a hydrocarbon residue of 1-8 carbon atoms, R.sub.2 is hydrogen or lower alkyl and rings A and B are unsubstituted or substituted by nitro, trifluoromethyl, halogen, lower alkyl or lower alkoxy, the nitrogen atom in the 5-position being unsubstituted or substituted by an oxygen atom, useful as muscle relaxants, anticonvulsants, sedatives and tranquilizing agents, and processes for production thereof. Also provided are novel intermediates of the general formula ##STR2## where R.sub.2 has the above meaning, rings A and B are unsubstituted or substituted as above and the nitrogen atom in the 4-position is unsubstituted or substituted by an oxygen atom.

公开(公告)号：US4082764A

公开(公告)日：1978-04-04

申请号：US612745

申请日：1975-09-12

申请人： Yutaka Kuwada ,  Kanji Meguro ,  Hiroyuki Tawada

发明人： Yutaka Kuwada ,  Kanji Meguro ,  Hiroyuki Tawada

IPC分类号： A61K20060101 ,  A61K31/55 ,  C07D20060101 ,  C07D239/92 ,  C07D243/00 ,  C07D249/00 ,  C07D249/08 ,  C07D487/04

CPC分类号： C07D239/92 ,  C07D249/08 ,  C07D487/04

摘要： The title compounds are prepared by reacting a 3-amino-3,4-dihydro-4-hydroxy-4-phenylquinazoline with a reactive derivative of a halogenoacetic acid, reacting the resultant halogenoacetyl derivative with a weak acid, reacting the resultant 2-(3-halomethyl-s-triazol-4-yl)benzophenone with hydroxylamine and subjecting the resultant 2-(3-hydroxyamino-methyl-s-triazol-4-yl)benzophenone to dehydration to effect ring closure.

公开(公告)号：US4002638A

公开(公告)日：1977-01-11

申请号：US505088

申请日：1974-09-11

申请人： Yutaka Kuwada ,  Hiroyuki Tawada ,  Kanji Meguro

发明人： Yutaka Kuwada ,  Hiroyuki Tawada ,  Kanji Meguro

IPC分类号： C07D487/04 ,  C07D249/12

CPC分类号： C07D487/04 ,  Y10S514/906 ,  Y10S514/96

摘要： Novel benzazepine derivatives of the formula ##STR1## wherein ring A is unsubstituted or substituted by halogen, nitro, alkyl, alkoxy or trifluoromethyl, R is hydrogen or alkyl which may be substituted, X is oxygen or sulfur and Y is -CH.sub.2 -CH.sub.2 - or -CH=CH-, and their pharmaceutically acceptable salts, exhibit excellent pharmacological activities such as analgetic and muscle relaxing activities.

摘要翻译： 式A的新的苯并氮杂衍生物，其中环A未被取代或被卤素，硝基，烷基，烷氧基或三氟甲基取代，R是氢或可被取代的烷基，X是氧或硫，Y是-CH 2 -CH 2 - 或-CH = CH-及其药学上可接受的盐，表现出优异的药理活性，例如止痛和肌肉松弛活性。

公开(公告)号：US4079060A

公开(公告)日：1978-03-14

申请号：US727382

申请日：1976-09-27

申请人： Yutaka Kuwada ,  Kanji Meguro ,  Yoshiaki Sato ,  Takeshi Fugono

发明人： Yutaka Kuwada ,  Kanji Meguro ,  Yoshiaki Sato ,  Takeshi Fugono

IPC分类号： C07D495/04 ,  C07D495/14

CPC分类号： C07D495/04

摘要： Novel thienopyridine-carboxylic acid derivatives, which are shown by the general formula ##STR1## wherein R.sup.1 represents hydrogen or a lower alkyl; R.sup.2 represents hydrogen, a lower alkyl or a halogen, or R.sup.1 and R.sup.2, taken together, may represent an alkylene to form a 5- or 6-membered ring with or without alkyl substituents; each of R.sup.4 and R.sup.5 represents hydrogen or a lower alkyl; and their pharmaceutically acceptable salts obtainable when R.sup.4 is hydrogen, which are useful medicines such as chemotherapeutic agents of bacterial infections.

摘要翻译： 新的噻吩并吡啶 - 羧酸衍生物，其通式为：其中R 1表示氢或低级烷基; R 2表示氢，低级烷基或卤素，或者R 1和R 2一起可以表示亚烷基以形成具有或不具有烷基取代基的5-或6-元环; R 4和R 5各自表示氢或低级烷基; 以及当R4为氢时可获得的药学上可接受的盐，其为有用的药物，例如细菌感染的化学治疗剂。

公开(公告)号：US4046772A

公开(公告)日：1977-09-06

申请号：US566434

申请日：1975-04-09

申请人： Yutaka Kuwada ,  Hiroyuki Tawada ,  Kanji Meguro

发明人： Yutaka Kuwada ,  Hiroyuki Tawada ,  Kanji Meguro

IPC分类号： A61K31/55 ,  A61P21/02 ,  A61P25/08 ,  A61P25/20 ,  B23B33/00 ,  C07D487/04 ,  C07D487/14

CPC分类号： C07D487/04 ,  B23B33/005 ,  Y10S514/906 ,  Y10S514/96

摘要： A benzodiazepine derivative of the general formula: ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group or a carboxyl group which may be esterified or amidated; R represents a hydrogen atom, an acyl group or a lower alkyl group, and each of the rings A and B is unsubstituted or substituted by halogen atom, nitro, lower alkyl, trifluoromethyl or lower alkoxy group, or its pharmaceutically acceptable acid addition salt is found to be useful as medicine in human and animal therapy, which acts on the central nervous system, e.g. muscle relaxants, anticonvulsants, sedatives, tranquilizers etc.

摘要翻译： 一种通式如下的苯并二氮杂衍生物：其中R 1表示氢原子，烷基或可被酯化或酰胺化的羧基; R表示氢原子，酰基或低级烷基，环A和B各自未被取代或被卤素原子，硝基，低级烷基，三氟甲基或低级烷氧基取代，或其药学上可接受的酸加成盐是 被发现在人和动物治疗中用作中枢神经系统的药物，例如 肌肉松弛剂，抗惊厥药，镇静剂，止痛药等。

公开(公告)号：US4017620A

公开(公告)日：1977-04-12

申请号：US575727

申请日：1975-05-08

申请人： Yutaka Kuwada ,  Kanji Meguro ,  Hiroyuki Tawada ,  Takashi Sohda ,  Hideaki Natsugari ,  Yoshiaki Sato

发明人： Yutaka Kuwada ,  Kanji Meguro ,  Hiroyuki Tawada ,  Takashi Sohda ,  Hideaki Natsugari ,  Yoshiaki Sato

IPC分类号： A61K31/55 ,  A61P25/00 ,  A61P25/20 ,  C07D495/14

CPC分类号： C07D495/14

摘要： There is disclosed new thienodiazepine derivatives of the general formula: ##STR1## wherein R.sup.1 represents a carboxyl group which may be esterified or amidated; each of R.sup.2 and R.sup.3 represents hydrogen atom or a lower alkyl group, or R.sup.2 and R.sup.3 may bond to each other to form an alkylene group; R.sup.4 represents a phenyl group which may have substituent; and R represents hydrogen atom, an acyl group or an alkyl group, or its pharmaceutically acceptable acid addition salts. The above compounds are useful as medicine in human and animal therapy, which act on the central nervous system, for example, as muscle relaxants, anticonvulsants, sedatives, minor tranquilizers, etc.

摘要翻译： 公开了以下通式的新的噻吩并二氮杂衍生物：其中R 1表示可被酯化或酰胺化的羧基; R 2和R 3各自表示氢原子或低级烷基，或者R 2和R 3可以彼此键合形成亚烷基; R4表示可以具有取代基的苯基; R表示氢原子，酰基或烷基，或其药学上可接受的酸加成盐。 上述化合物可用作人和动物治疗中的药物，其作用于中枢神经系统，例如肌肉松弛剂，抗惊厥药，镇静剂，微量镇静剂等。

公开(公告)号：US4013763A

公开(公告)日：1977-03-22

申请号：US592814

申请日：1975-07-03

申请人： Yutaka Kuwada ,  Kanji Meguro ,  Hideaki Natsugari ,  Yoshiaki Sato ,  Hiroyuki Tawada

发明人： Yutaka Kuwada ,  Kanji Meguro ,  Hideaki Natsugari ,  Yoshiaki Sato ,  Hiroyuki Tawada

IPC分类号： C07D213/50 ,  C07D249/08 ,  C07D487/14 ,  C07D498/14 ,  C07D491/22

CPC分类号： C07D249/08 ,  C07D213/50 ,  C07D487/14

摘要： A novel heterocyclic compound of the general formula: ##STR1## wherein R.sup.1 represents hydrogen atom or a hydrocarbon residue; R.sup.2 represents hydrogen atom or a lower alkyl group; Py represents a pyridyl group; Y represents an ethylene or a trimethylene group which may have lower alkyl group as substituent; Z represents oxygen atom, sulfur atom or --NH-- groups; and the ring A is either unsubstituted or substituted by a halogen atom, nitro, alkyl, alkoxy or trifluoromethyl group, is found to be useful as medicine in human and animal therapy, as these compounds act on the central nervous system, as, for example, muscle relaxants, anticonvulsants, sedatives, minor tranquilizers, etc.